A novel LDL-mimic nanocarrier for the targeted delivery of curcumin into the brain to treat Alzheimer's disease

Meng, Fanfei; Asghar, Sajid; Gao, Shiya; Su, Zhigui; Song, Jue; Huo, Meirong; Meng, Weidong; Ping, Qineng; Xiao, Yanyu

doi:10.1016/j.colsurfb.2015.06.025

Cited by 154 publications

(73 citation statements)

References 47 publications

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“…31 Moreover, the presence of PEG chains in the S100-TCA would also restrict the size of NLCs. 19 All Cur-loaded NLCs showed good monodispersity, as a PDI value ,0.3 has been associated with narrow particle-size distribution. 32 The substantial increase in PDI value for a higher S100-TCA level (100 mg) was attributed to the excess S100-TCA that failed to get completely adsorbed on to the NLCs and could have assembled into the small sized, thus leading to the increased PDI value.…”

Section: Results and Discussion S100-tca Synthesis And Characterizationmentioning

confidence: 99%

“…19 To obtain TCA, 2 mL distilled water containing 0.93 mmol TCA sodium salt was slowly dropped into hydrochloric acid solution (0.1 M, 3 mL) at 0°C and stirred at room temperature for 16 hours. Yellow crystalline mass was filtered using Whatman cellulose filters and vacuum-dried to obtain TCA.…”

Section: Synthesis Of S100-tcamentioning

confidence: 99%

“…19 Briefly, 10 mL of ethanol-chloroform (1:1, v:v) was used to get a lipid-drug mixture of phosphatidylcholine (330 mg), cholesterol oleate (20 mg), glycerol trioleate (70 mg), and Cur (16 mg). A dried lipid film obtained through rotary evaporation at 37°C under vacuum was then hydrated with 10% (v:v) glycerol solution at 37°C for 30 minutes and subjected to ultrasonication for 5 minutes at 300 W in an ice bath.…”

Section: Preparation Of Cur-tca Nlcsmentioning

confidence: 99%

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Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

Tian¹,

Asghar²,

Wu³

et al. 2017

IJN

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The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (−7 to −3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs.

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Section: Results and Discussion S100-tca Synthesis And Characterizationmentioning

confidence: 99%

Section: Synthesis Of S100-tcamentioning

confidence: 99%

Section: Preparation Of Cur-tca Nlcsmentioning

confidence: 99%

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Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

Tian¹,

Asghar²,

Wu³

et al. 2017

IJN

Self Cite

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“…Synthesis of N-acetyl-L-cysteine-polyethylene glycol (100)-monostearate (NAPG) NAPG was synthesized according to a previous research with some modifications (Meng et al, 2015). Briefly, NAC (1 mmol) was dissolved in anhydrous N,N-dimethylformamide (5 mL) and then 0.63 mmol EDCI was added.…”

Section: Animalsmentioning

confidence: 99%

“…Cur-loaded NLC (Cur-NLC) was prepared by a solvent evaporation method as described by Meng et al (2015). Briefly, lipid matrix materials (330 mg of PC, 20 mg of cholesterol oleate, 70 mg of glycerol trioleate) and Cur (16 mg) were dissolved in 10 mL of ethanol-chloroform mixture (1:1, v/v) and dried in a rotary evaporator under vacuum at 40 C for 4 h. The dried lipid film was hydrated with 10 mL 10% (v/v) glycerol solution at 37 C for 30 min, then ultrasonicated at 300 W for 5 min, followed by extrusion through 0.45 mm cellulose nitrate membrane to remove the unentrapped Cur and obtain Cur-NLC.…”

Section: Preparation Of Cur-napg-nlcmentioning

confidence: 99%

N-acetyl-L-cysteine functionalized nanostructured lipid carrier for improving oral bioavailability of curcumin: preparation, in vitro and in vivo evaluations

Tian

Asghar

et al. 2017

Drug Delivery

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The application of orally administered nanoparticles in the circulation system is limited by the secretion and shedding of intestinal tract mucous layer. In order to enhance mucoadhesion and mucus penetration of curcumin (Cur)-loaded nanostructured lipid carrier (NLC) after oral administration, a new multifunctional conjugate, N-acetyl-L-cysteine-polyethylene glycol (100)-monostearate (NAPG), was synthesized. Functionalized nanocarriers (Cur-NAPG-NLC) modified by different amounts of NAPG (the amounts of NAPG were 20, 50, and 100 mg) were prepared and investigated for in vitro and in vivo behavior. Mean particle sizes of 89-141 nm with negative zeta potential (À15 to À11 mV) and high encapsulation efficiency (EE, >90%) possessing spherical and stable nanocarriers were observed. Sustained drug release was also observed for the NAPG-NLC. In situ intestinal perfusion studies showed that with increasing the amount of NAPG increase absorption of Cur. In vivo oral pharmacokinetic evaluation suggested that the bioavailability of Cur in rats was proportional to the degree of functionalization of NLCs with NAPG. AUC 0-t of Cur-NAPG100-NLC was improved by 499.45 and 116.89 folds as compared to that of Cur solution and unmodified Cur-NLC, respectively. In conclusion, NAPG modified NLC could be a promising drug delivery system for improving oral performance of BCS class IV drugs.ARTICLE HISTORY

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Potential Use of Curcuminoids for the Treatment of Alzheimer's Disease

Ahmed

Javed

Tariq

et al. 2017

Neuroprotective Effects of Phytochemicals in Neurological Disorders

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A novel LDL-mimic nanocarrier for the targeted delivery of curcumin into the brain to treat Alzheimer's disease

Cited by 154 publications

References 47 publications

Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

N-acetyl-L-cysteine functionalized nanostructured lipid carrier for improving oral bioavailability of curcumin: preparation, in vitro and in vivo evaluations

Potential Use of Curcuminoids for the Treatment of Alzheimer's Disease

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